AR061010A1 - DERIVATIVES OF TRIAZOL I I - Google Patents

DERIVATIVES OF TRIAZOL I I

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Publication number
AR061010A1
AR061010A1 ARP070102142A ARP070102142A AR061010A1 AR 061010 A1 AR061010 A1 AR 061010A1 AR P070102142 A ARP070102142 A AR P070102142A AR P070102142 A ARP070102142 A AR P070102142A AR 061010 A1 AR061010 A1 AR 061010A1
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Argentina
Prior art keywords
het
replaced
hal
atoms
groups
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ARP070102142A
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Spanish (es)
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Eggenweiler Hans-Michael Dr
Wolf Michael Dr
Buchstaller Hans-Peter Dr
Christian Sirrenberg
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Merck Patent Gmbh
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38189162&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR061010(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR061010A1 publication Critical patent/AR061010A1/en

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Abstract

Los derivados de triazol de la formula (1) en donde R1 es OH, OCH3, OCF3, OCHF2, OBzl, OAc, p-metoxibenciloxi, SH, S(O)mCH3, SO2NH2, Hal, CF3 o CH3; R2 es CONA[(CH2)oAr], CONA[(CH2)oHet'], SO2NA[(CH2)oAr'] o SO2NA[(CH2)oHet']; R3 es H, Hal, CN, NO2, A, Alk, (CH2)nAr, (CH2)nHet', COOH, COOA, COOAr, COOHet', CONH2, CONHA, CONAA', CONHAr, CONAAr, CON(Ar)2, CONHHet', CON(Het')2, NH2, NHA, NHAr, NHHet', NAA', NHCOA, NACOA', NHCOAr, NHCOHet', NHCOOA, NHCOOAr, NHCOOHet', NHCONHA, NHCONHAr, NHCONHHet', OH, OA, OAr, OHet', SH, S(O)mA, S(O)mAr, S(O)mHet', SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet', SO2NAHet', SO2NA-bencilo, SO2N(Ar)2 o SO2N(Het')2; R4, R5, R6 son en cada caso, de modo independiente entre sí, H, Hal, CN, NO2, A, Alk, (CH2)nAr, (CH2)nHet', COOH, COOA, COOAr, COOHet', CONH2, CONHA, CONAA', CONHAr, CONAAr, CON(Ar)2, CONHHet', CON(Het')2, NH2, NHA, NHAr, NHHet', NAA', NHCOA, NHCONH2, NACOA', NHCO(CH2)nAr, NHCOHet', NHCOOA, NHCOOAr, NHCOOHet', NHCONHA, NHCONHAr, NHCONHHet', OH, OA, O(CH2)oHet, O(CH2)oNH2, O(CH2)oCN, OAr, OHet', SH, S(O)mA, S(O)mAr, S(O)mHet', SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet', SO2N(Ar)2 o SO2N(Het')2; R4 y R5 también son juntos OCH2O, OCH2CH2O, -CH=CH-CH=CH-, NH-CH=CH o CH=CH-NH; Y es OH o SH; A, A' son en cada caso, de modo independiente entre sí, alquilo no ramificado o ramificado C1-10, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR8 y/o por grupos -CH=CH y/o también 1-5 átomos de H pueden estar reemplazados por F, Cl, Br y/o R7, Alk o alquilo cíclico C3-7; A y A' también son juntos una cadena de alquileno C2-6, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Alk es alquenilo C2-6; R7 es CN, COOR9, CONR9R10, NR9R10, NHCOR9, NHCOOR9 u OR9; R8 es cicloalquilo C3-7, cicloalquilalquileno C4-10, Alk o alquilo no ramificado o ramificado C1-6, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH y/o también 1-5 átomos de H pueden estar reemplazados por F y/o Cl; R9, R10 son en cada caso, de modo independiente entre sí, H o alquilo C1-5, en donde 1-3 grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe o Net y/o también 1- 5 átomos de H pueden estar reemplazados por F y/o Cl; R9 y R10 también son juntos una cadena de alquileno C2-6, en donde un grupo CH2 puede estar reemplazado por O, S, SO, SO2, NH, NR8, NCOR8 o NCOOR8; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, XR7, Y, CN, fenilo, Het'', OXHet''', OA, OXR7, S(O)mA, S(O)mXR7, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10 y/o NR9SO2R10; Ar' es fenilo, naftilo o bifenilo mono-, di- o trisustituido con Hal, A, XR7, XR4, Y, CN, Ar, Het, OA, OXR7, OXR4, S(O)mA, S(O)mXR7, S(O)mXR4, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, y/o NR9SO2R10; Het es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, XR7, Y, CN, Ar, OA, OXR7, S(O)mA, S(O)mXR7, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, NR9SO2R10, =S, =NR11, =NR11R7 y/u =O (oxígeno del carbonilo); Het' es un heterociclo mono- o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, XR7, XR4, Y, CN, Ar, Het, OA, OXR7, OXR4, S(O)mA, S(O)mXR7, S(O)mXR4, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, NR9SO2R10, =S, =NR11, =NR11R7 y/u =O (oxígeno del carbonilo), y/o en donde un nitrogeno del anillo puede estar sustituido con -O-; Het'' es un heterociclo aromático monocíclico con 1 a 3 átomos de N, O y/o S; Het''' es un heterociclo saturado monocíclico con 1 a 3 átomos de N, O y/o S; X es alquileno no ramificado o ramificado C1-10, en donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NR8 y/o por grupos -CH=CH y/o también 1-5 átomos de H pueden estar reemplazados por F, Cl, Br y/o R7; R11 es H o A; Hal es F, Cl, Br o I; m es 0, 1 o 2; n es 0, 1, 2, 3 o 4; o es 1, 2 o 3; así como sus derivados, sales, solvatos, tautomeros y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la HSP90 y pueden ser utilizados para preparar un medicamento para el tratamiento de enfermedades en las que la inhibicion, la regulacion y/o la modulacion de la HSP90 desempena un papel importante. utiles para enfermedades tumorales, virales, inflamatorias, angiogenesis, fibrogenesis.The triazole derivatives of the formula (1) wherein R1 is OH, OCH3, OCF3, OCHF2, OBzl, OAc, p-methoxybenzyloxy, SH, S (O) mCH3, SO2NH2, Hal, CF3 or CH3; R2 is CONA [(CH2) oAr], CONA [(CH2) oHet '], SO2NA [(CH2) oAr'] or SO2NA [(CH2) oHet ']; R3 is H, Hal, CN, NO2, A, Alk, (CH2) nAr, (CH2) nHet ', COOH, COOA, COOAr, COOHet', CONH2, CONHA, CONAA ', CONHAr, CONAAr, WITH (Ar) 2 , CONHHet ', WITH (Het') 2, NH2, NHA, NHAr, NHHet ', NAA', NHCOA, NACOA ', NHCOAr, NHCOHet', NHCOOA, NHCOOAr, NHCOOHet ', NHCONHA, NHCONHAr, NHCONHHet', OH, OA , OAr, OHet ', SH, S (O) mA, S (O) mAr, S (O) mHet', SO2NH2, SO2NHA, SO2NAA ', SO2NHAr, SO2NAAr, SO2NHHet', SO2NAHet ', SO2NA-benzyl, SO2N ( Ar) 2 or SO2N (Het ') 2; R4, R5, R6 are in each case, independently of each other, H, Hal, CN, NO2, A, Alk, (CH2) nAr, (CH2) nHet ', COOH, COOA, COOAr, COOHet', CONH2, CONHA, CONAA ', CONHAr, CONAAr, WITH (Ar) 2, CONHHet', WITH (Het ') 2, NH2, NHA, NHAr, NHHet', NAA ', NHCOA, NHCONH2, NACOA', NHCO (CH2) nAr, NHCOHet ', NHCOOA, NHCOOAr, NHCOOHet', NHCONHA, NHCONHAr, NHCONHHet ', OH, OA, O (CH2) oHet, O (CH2) oNH2, O (CH2) oCN, OAr, OHet', SH, S (O) mA, S (O) mAr, S (O) mHet ', SO2NH2, SO2NHA, SO2NAA', SO2NHAr, SO2NAAr, SO2NHHet ', SO2N (Ar) 2 or SO2N (Het') 2; R4 and R5 are also together OCH2O, OCH2CH2O, -CH = CH-CH = CH-, NH-CH = CH or CH = CH-NH; Y is OH or SH; A, A 'are in each case, independently of each other, C1-10 unbranched or branched alkyl, wherein one, two or three CH2 groups may be replaced by O, S, SO, SO2, NH, NR8 and / or by groups -CH = CH and / or also 1-5 H atoms can be replaced by F, Cl, Br and / or R7, Alk or C3-7 cyclic alkyl; A and A 'are also together a C2-6 alkylene chain, where a CH2 group can be replaced by O, S, SO, SO2, NH, NR8, NCOR8 or NCOOR8; Alk is C2-6 alkenyl; R7 is CN, COOR9, CONR9R10, NR9R10, NHCOR9, NHCOOR9 or OR9; R8 is C3-7 cycloalkyl, C4-10 cycloalkylalkylene, Alk or C1-6 unbranched or branched alkyl, wherein one, two or three CH2 groups may be replaced by O, S, SO, SO2, NH and / or also 1 -5 atoms of H may be replaced by F and / or Cl; R9, R10 are in each case, independently of each other, H or C1-5 alkyl, wherein 1-3 CH2 groups may be replaced by O, S, SO, SO2, NH, NMe or Net and / or also 1 - 5 atoms of H may be replaced by F and / or Cl; R9 and R10 are also together a C2-6 alkylene chain, where a CH2 group may be replaced by O, S, SO, SO2, NH, NR8, NCOR8 or NCOOR8; Ar is phenyl, naphthyl or biphenyl unsubstituted or mono-, di- or trisubstituted with Hal, A, XR7, Y, CN, phenyl, Het '', OXHet '' ', OA, OXR7, S (O) mA, S (O) mXR7, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10 and / or NR9SO2R10; Ar 'is phenyl, naphthyl or biphenyl mono-, di- or trisubstituted with Hal, A, XR7, XR4, Y, CN, Ar, Het, OA, OXR7, OXR4, S (O) mA, S (O) mXR7, S (O) mXR4, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, and / or NR9SO2R10; Het is a saturated, unsaturated or aromatic mono- or bicyclic heterocycle with 1 to 4 atoms of N, O and / or S that may not be substituted or that may be mono-, di- or trisubstituted with Hal, A, XR7, Y , CN, Ar, OA, OXR7, S (O) mA, S (O) mXR7, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, NR9SO2R10, = S, NR2R11 = S, NR11R7 and / u = O (carbonyl oxygen); Het 'is a saturated, unsaturated or aromatic mono- or bicyclic heterocycle with 1 to 4 atoms of N, O and / or S that may not be substituted or that may be mono-, di- or trisubstituted with Hal, A, XR7, XR4, Y, CN, Ar, Het, OA, OXR7, OXR4, S (O) mA, S (O) mXR7, S (O) mXR4, NO2, NH2, NR9R10, NR8R9, CONR9R10, CONR8R9, SO2NR9R10, SO2NR8R9, NR9COR10, NR9CONR9R10, NR9SO2R10, = S, = NR11, = NR11R7 and / u = O (carbonyl oxygen), and / or where a ring nitrogen can be substituted with -O-; Het '' is a monocyclic aromatic heterocycle with 1 to 3 atoms of N, O and / or S; Het '' 'is a monocyclic saturated heterocycle with 1 to 3 atoms of N, O and / or S; X is C1-10 unbranched or branched alkylene, wherein one, two or three CH2 groups may be replaced by O, S, SO, SO2, NH, NR8 and / or by groups -CH = CH and / or also 1- 5 atoms of H may be replaced by F, Cl, Br and / or R7; R11 is H or A; Hal is F, Cl, Br or I; m is 0, 1 or 2; n is 0, 1, 2, 3 or 4; or is 1, 2 or 3; as well as its derivatives, salts, solvates, tautomers and stereoisomers of pharmaceutical utility, including their mixtures in all proportions. They are inhibitors of HSP90 and can be used to prepare a medicament for the treatment of diseases in which the inhibition, regulation and / or modulation of HSP90 plays an important role. Useful for tumor, viral, inflammatory, angiogenesis, fibrogenesis diseases.

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